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. Author manuscript; available in PMC: 2021 Mar 26.
Published in final edited form as: J Med Chem. 2020 Mar 10;63(6):2854–2876. doi: 10.1021/acs.jmedchem.9b01189

Table 7.

In Vitro Activity of Stage III Analogues

graphic file with name nihms-1577324-t0029.jpg
Compound X R1 R2 R3 R4 Ratio (5/50)a Fold-Signalb EC50 hPPARα (μM)c
20 COOH 4-Cl 3-Me H H 1.2 1.2 0.029±0.001
21 COOH 4-Br 3-Me H H 1.2 1.3 0.031±0.008
22 COOH 4-I 3-Me H H 1.8 1.5 0.027±0.003
23 COOH 2,4-difluoro 3-Me H H 1.2 1.4 0.056±0.007
24 COOH 3,4-difluoro 3-Me H H 1.4 1.6 0.018±0.001
25 COOH 3,5-difluoro 3-Me H H 1.1 1.6
26 COOH 4-F 3-F H H 0.7 1.7
27 COOH 4-F 3-Cl H H 1.1 1.5
28 COOH 4-OPFB 3-OPFB H H 1.0 1.4 0.81±0.17
29 COOH 4-OPFB 2-OPFB H H 0.9 1.2 0.93±0.02
30 COOH 4-F 3-Me H Me 0.8 2.1 0.067±0.01
31 COOH 4-F 3-Me F H 0.9 1.5 0.040±0.001
32 COOH 4-F 3-Cl F H 1.1 1.8 0.052±0.011
33 OC(CH3)2COOH 4-F 3-Me H H 1.0 1.6 0.74±0.04
4b 0.8 1.3 0.77±0.03
4a (A91) 0.5 1.4 4.43±0.01
GW590735 1.0 1.0 0.015±0.002
a

Ratio of relative light unit (RLU) signal at 5 μM and 50 μM compound concentrations.

b

Ratio of signal maximal signal (RLU) strength observed for the compound of interest to that obtained with GW590735.

c

EC50 values represent the mean ± SEM of atleast two separate experiments performed in triplicate. OPFB = para-fluorobenzyl. Numbering shown is based on the name of the resulting products. Blank cells indicate compound was not selected for testing in the corresponding assay.